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Akademický článek

Characterization of interactions between hepatitis C virus NS5B polymerase, annexin A2 and RNA – effects on NS5B catalysis and allosteric inhibition

Autor: Sara M. Ø. Solbak, Eldar Abdurakhmanov, Anni Vedeler, U. Helena Danielson

Publikováno v: Virology Journal, Vol 14, Iss 1, Pp 1-11 (2017)

Abstract Background Direct acting antivirals (DAAs) provide efficient hepatitis C virus (HCV) therapy and clearance for a majority of patients, but are not available or effective for all patients. They risk developing HCV-induced hepatocellular carci

Externí odkaz: https://doaj.org/article/55b8ebab05a845dda7c6c094c3087697

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Characterization of interactions between hepatitis C virus NS5B polymerase, annexin A2 and RNA – effects on NS5B catalysis and allosteric inhibition

Autor: Solbak, Sara M.Ø., Abdurakhmanov, Eldar, Vedeler, Anni, Danielson, U. Helena

Publikováno v: Virology Journal, Vol 14, Iss 1, Pp 1-11 (2017)

Background Direct acting antivirals (DAAs) provide efficient hepatitis C virus (HCV) therapy and clearance for a majority of patients, but are not available or effective for all patients. They risk developing HCV-induced hepatocellular carcinoma (HCC

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::71f52348006a9c8b1fc772f514dbdafd
http://link.springer.com/article/10.1186/s12985-017-0904-4

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Synthesis of Filibuvir. Part II. Second-Generation Synthesis of a 6,6-Disubstituted 2H-Pyranone via Dieckmann Cyclization of a β-Acetoxy Ester

Autor: Stuart Taylor, Gregory W. Sluggett, Brian G. Conway, Leo Joseph Letendre, Robert A. Singer, Nicola Mawby, Kevin Meldrum, Jon Blunt, Zhihui Peng, Kyle R. Leeman, John A. Ragan, Holly Strohmeyer, Eric M. Cordi, Li-Jen Ping, Janice E. Sieser, Roberto Colon-Cruz, Brian C. Vanderplas

Publikováno v: Organic Process Research & Development. 18:36-44

This paper describes an improved sequence for the conversion of an oxazolidinone (3) to a β-keto lactone (5). The primary drivers behind this change were the modest and variable yields observed in the intramolecular cyclization to generate the β-ke

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::249802ea1a0efa9c951d4e02f1bee3a6
https://doi.org/10.1021/op400236r

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Non-nucleoside Analogue Polymerase Inhibitors in Development

Autor: Paul J. Pockros

Publikováno v: Clinics in Liver Disease. 17:123-128

Non-nucleoside polymerase inhibitors have several limitations including low to moderate potency, a low barrier to resistance, unlikely to cross genotype activity, genotype potency 1b > 1a, and hyperbilirubinemia for 2 of the drugs (tegobuvir and BI-2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bbbdcca37356b7cc9868323ed7e9f98
https://doi.org/10.1016/j.cld.2012.09.004

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Discontinued drugs in 2012 - 2013: hepatitis C virus infection

Autor: Emanuela Zappulo, Guglielmo Borgia, Antonio Riccardo Buonomo, Ivan Gentile

Publikováno v: Expert opinion on investigational drugs. 24(2)

Hepatitis C virus (HCV) chronically infects about 150 million people worldwide. Antiviral treatment can stop and even reverse the progression of the disease. Several antivirals have been developed. However, about 10,000 compounds are tested for each

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44043828634b2fe43a176e5efd71566b
https://pubmed.ncbi.nlm.nih.gov/25384989

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Determination and control of TEMPO, a potentially genotoxic free radical reagent used in the synthesis of filibuvir

Autor: Gregory W. Sluggett, Holly Strohmeyer

Publikováno v: Journal of pharmaceutical and biomedical analysis. 62

The synthesis of filibuvir, a hepatitis C virus polymerase inhibitor candidate, involves use of 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO), a potentially genotoxic free radical reagent. A headspace gas chromatographic method utilizing selected-ion

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9560fa7e95b323f48a9dcd4a72aee432
https://pubmed.ncbi.nlm.nih.gov/22269174

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Synthesis of Filibuvir

Autor: J A Ragan, Philip Kocienski, N D Ide

Publikováno v: Synfacts. 10:0342-0342

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3c739778fd4a88a2e9aa122f6a7a09d0
https://doi.org/10.1055/s-0033-1340875

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286 EXPOSURE-RESPONSE RELATIONSHIP OF FILIBUVIR IN HCV INFECTED PATIENTS: APPLICATION TO DOSE SELECTION FOR COMBINATION THERAPY

Autor: J. Hammond, V.S. Purohit, M. O'Gorman, S. Neelakantan, T.G. Tensfeldt

Publikováno v: Journal of Hepatology. 52:S119-S120

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1470ac400f5abde5187835db9a53c811
https://doi.org/10.1016/s0168-8278(10)60288-7

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1052 ANTIVIRAL ACTIVITY OF FILIBUVIR IN COMBINATION WITH PEGYLATED INTERFERON ALFA-2A AND RIBAVIRIN FOR 28 DAYS IN TREATMENT NAIVE PATIENTS CHRONICALLY INFECTED WITH HCV GENOTYPE 1

Autor: R. Pruitt, E.J. Lawitz, K. Durham, J. Lalezari, Subasree Srinivasan, Ira M. Jacobson, J. Hammond, E. DeJesus, Claudia Martorell, M. Rosario, F. Haas, Maribel Rodriguez-Torres, S. Jagannatha, Paul J. Pockros

Publikováno v: Journal of Hepatology. 50:S382-S383

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b360ba3a5a22dc1e65163736cf14d5cc
https://doi.org/10.1016/s0168-8278(09)61054-0

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